CAY10790 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50 = 2.8 µM) and G protein-coupled bile acid receptor 1 (GPBAR1) agonist. It induces receptor transactivation in HEK293T cells expressing human GPBAR1 (EC50 = 3 µM). CAY10790 (10 µM) reduces TNF-alpha and IL-1beta levels in LPS-stimulated RAW...

FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A (Cay-12088) and rapamycin (Cay-13346). Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the...